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426100 Lactacystin, Synthetic - CAS 1258004-00-0 - Calbiochem

Lactacystin, Synthetic, CAS 1258004-00-0, is an irreversible inhibitor of 20S proteasome inhibitor (IC₅₀ = 500 nM). A covalent inhibitor of the chymotrypsin & trypsin-like activities of proteasome.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Proteasome Inhibitor VI

Primary Target: 20S proteasome (MCP; multicatalytic proteinase complex)
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426100
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1258004-00-0C₁₅H₂₄N₂O₇S

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426100-1MG
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      426100-200UG
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          		 Plastic ampoule 200 μg
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          426100-400UG
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              Description
              OverviewAn irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex) (IC50 = 500 nM for 20S proteasome). Blocks proteasome activity by targeting the catalytic β-subunit. Acts as a covalent inhibitor of the chymotrypsin- and trypsin-like activities of the proteasome. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells and inhibits progression of synchronized Neuro 2A cells and MG-63 human osteosarcoma cells beyond the G1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 µM).
              Catalogue Number426100
              Brand Family Calbiochem®
              SynonymsProteasome Inhibitor VI
              References
              ReferencesKeyomarsi, K., et al. 2011. Cell. Biol. Toxicol. 27, 123.
              Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem. 31, 279.
              Dick, L.R., et al. 1996. J. Biol. Chem. 271, 7273.
              Oda, K., et al. 1996. Biochem. Biophys. Res. Commun. 219, 800.
              Fenteany, G., et al. 1995. Science 268, 726.
              Imajoh-Ohmi, S., et al. 1995. Biochem. Biophys. Res. Commun. 217, 1070.
              Jensen, T.J., et al. 1995. Cell 83, 129.
              Katagiri, M.M., et al. 1995. J. Antibiot. 48, 344.
              Mori, S., et al. 1995. J. Biol. Chem. 270, 29447.
              Tanaka, H., et al. 1995. Biochem. Biophys. Res. Commun. 216, 291.
              Fenteany, G., et al. 1994. Proc. Natl. Acad. Sci. USA 91, 3358.
              Omura, S., et al. 1991. J. Antibiot. 44, 117.
              Product Information
              CAS number1258004-00-0
              ATP CompetitiveN
              FormWhite solid
              Hill FormulaC₁₅H₂₄N₂O₇S
              Chemical formulaC₁₅H₂₄N₂O₇S
              ReversibleN
              Structure formula ImageStructure formula Image
              Quality LevelMQ100
              Applications
              Biological Information
              Primary Target20S proteasome (MCP; multicatalytic proteinase complex)
              Primary Target IC<sub>50</sub>500 nM against 20S proteasome; 10 µM against NF-κB activation
              Purity≥99% by HPLC
              Physicochemical Information
              Cell permeableN
              Dimensions
              Materials Information
              Toxicological Information
              Safety Information according to GHS
              Safety Information
              Product Usage Statements
              Storage and Shipping Information
              Ship Code Ambient Temperature Only
              Toxicity Standard Handling
              Storage -20°C
              Do not freeze Ok to freeze
              Special InstructionsFollowing reconstitution in DMSO, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Unstable in aqueous solutions; reconstitute in H₂O just prior to use.
              Packaging Information
              Transport Information
              Supplemental Information
              Specifications
              Global Trade Item Number
              Catalogue Number GTIN
              426100-1MG 04055977187311
              426100-200UG 04055977187328
              426100-400UG 04055977187335

              Documentation

              Lactacystin, Synthetic - CAS 1258004-00-0 - Calbiochem MSDS

              Title

              Safety Data Sheet (SDS) 

              Lactacystin, Synthetic - CAS 1258004-00-0 - Calbiochem Certificates of Analysis

              TitleLot Number
              426100

              References

              Reference overview
              Keyomarsi, K., et al. 2011. Cell. Biol. Toxicol. 27, 123.
              Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem. 31, 279.
              Dick, L.R., et al. 1996. J. Biol. Chem. 271, 7273.
              Oda, K., et al. 1996. Biochem. Biophys. Res. Commun. 219, 800.
              Fenteany, G., et al. 1995. Science 268, 726.
              Imajoh-Ohmi, S., et al. 1995. Biochem. Biophys. Res. Commun. 217, 1070.
              Jensen, T.J., et al. 1995. Cell 83, 129.
              Katagiri, M.M., et al. 1995. J. Antibiot. 48, 344.
              Mori, S., et al. 1995. J. Biol. Chem. 270, 29447.
              Tanaka, H., et al. 1995. Biochem. Biophys. Res. Commun. 216, 291.
              Fenteany, G., et al. 1994. Proc. Natl. Acad. Sci. USA 91, 3358.
              Omura, S., et al. 1991. J. Antibiot. 44, 117.

              Brochure

              Title
              Caspases and other Apoptosis Related Tools Brochure
              Proteasomes Technical Bulletin

              Citations

              Title
            • Keyomarsi, K., et al. 2011. Cell. Biol. Toxicol. 27, 123.
            • Lacher, M.D., et al. 2006. Cancer Research 66, 1648.
            • Wu, C-J., et al. 2005. European Molecular Biology Organization Journal 24, 1886.
              		•
              Data Sheet

              Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

              Revision23-October-2012 JSW
              SynonymsProteasome Inhibitor VI
              DescriptionAn irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex) (IC50 = 500 nM for 20S proteasome). Blocks proteasome activity by targeting the catalytic β-subunit. Acts as a covalent inhibitor of the chymotrypsin and trypsin-like activities of the proteasome. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells beyond theG1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 µM)
              FormWhite solid
              CAS number1258004-00-0
              Chemical formulaC₁₅H₂₄N₂O₇S
              Structure formulaStructure formula
              Purity≥99% by HPLC
              SolubilityDMSO (50 mg/ml) or H₂O
              Storage -20°C
              Do Not Freeze Ok to freeze
              Special InstructionsFollowing reconstitution in DMSO, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Unstable in aqueous solutions; reconstitute in H₂O just prior to use.
              Toxicity Standard Handling
              ReferencesKeyomarsi, K., et al. 2011. Cell. Biol. Toxicol. 27, 123.
              Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem. 31, 279.
              Dick, L.R., et al. 1996. J. Biol. Chem. 271, 7273.
              Oda, K., et al. 1996. Biochem. Biophys. Res. Commun. 219, 800.
              Fenteany, G., et al. 1995. Science 268, 726.
              Imajoh-Ohmi, S., et al. 1995. Biochem. Biophys. Res. Commun. 217, 1070.
              Jensen, T.J., et al. 1995. Cell 83, 129.
              Katagiri, M.M., et al. 1995. J. Antibiot. 48, 344.
              Mori, S., et al. 1995. J. Biol. Chem. 270, 29447.
              Tanaka, H., et al. 1995. Biochem. Biophys. Res. Commun. 216, 291.
              Fenteany, G., et al. 1994. Proc. Natl. Acad. Sci. USA 91, 3358.
              Omura, S., et al. 1991. J. Antibiot. 44, 117.
              Citation
            • Keyomarsi, K., et al. 2011. Cell. Biol. Toxicol. 27, 123.
            • Lacher, M.D., et al. 2006. Cancer Research 66, 1648.
            • Wu, C-J., et al. 2005. European Molecular Biology Organization Journal 24, 1886.
              		•